PHARMACEUTICAL DOSAGE FORMS (DF)

REASONS FOR DOSAGE FORMULATION:

Administration
Appearance
Solubility/ Absorption
Stability
Taste
LIQUID DF

REASONS FOR LIQUID FORM:

Administration
Different Routes
Solubility/ Absorption

TYPES OF INSTABILITY:
1. Chemical
Hydrolysis
ex.: Pen G, Aspirin
Oxidation
Ingredients
Container
ex.: Leaching,
Sorption

2. Microbial

Raw Material
Packaging Material
Equipment
Personnel

Product
Natural
Oral (soln & susp)
Topical
Urethral, Vaginal, Rectal

PRESERVATIVES
5% Phenol/ Carbolic
acid
15% Ethanol
18% Ethanol
Parabens
Benzoic acid (0.1-0.2%)
Sorbic acid
Hexachlorophene
Hydrocinnamyl Alcohol
Quaternary Ammonium
Compounds
Isopropyl Alcohol

Effective for
(introduced by Lister)
Acidic prep.
Neutral & Alkaline prep.
pH 3-9
pH <4
pH <5 (antimycotic)
G+
P. aeruginosa
Ophthalmic Soln
(incompatible with soap)
External prep.

USP REQUIREMENT
Free from
Salmonella spp.
E. coli
P. aeruginosa (pyocyanin: blue-green pigment)
S. aureus (catalase )
Total microbial count

TYPES OF LIQUID DF:

1. SOLUTION
>METHODS OF PREPARATION:
a. Extraction
b. Chemical Reaction
ex.: Mg carbonate + citric acid Mg citrate + CO2 + H2O
c. Simple Solution- employs techniques to hasten dissolution;

heat
particle size reduction
solubilizing agent
vigorous agitation

A. AQUEOUS SOLUTIONS
1. Aromatic/ Medicated Waters
-clear; saturated with volatile substances
-for perfuming/flavoring
>>Method for preparation:
a. Distillation/ Cohobation: from fresh delicate drugs with small
quantity of volatile substance; ex: STRONGER ROSE WATER NF
b. Solution: 2mg/2mL volatile oil in 1mL purified H2O; stand
overnight then filter off excess oil

c. Alternate Solution: 2mg/mL volatile oil triturated with talc,

dissolved in H2O; filter
2. Diluted Acids
- %w/v when diluted; %w/w if concentrated
-prepared by diluting with purified H2O
3. Douches
- directed against a part or into body cavity; ex.:
a. Dobells Solution: nasal, pharyngeal; with Na borate
b. Benzalkonium Cl: vaginal
>>Types of Douches:
1. Ophthalmic

4. Urethral

2. Nasal

5. Vaginal

3. Pharyngeal
4. Enemas
-rectal injections; ex.:
a. Fleet enema: constipation & cleanse bowel; mono+dibasic NaPO 4
b. BaSO4 Enema: radiopaque; diagnostic aid
>> Types of Enema:
1. Retention: local & systemic effect
2. Evacuation: cleanse bowel
5. Gargles
-with antiseptics, antibiotics, anesthetics
-treat pharynx & nasopharynx; forces air from lungs, held in throat
6. Mouthwashes
- concentrated; therapeutic and cosmetic use; used by swishing
7. Juices
- from fresh ripe fruit; enzymatic reaction destroy pectin (makes juice
cloudy)
- as vehicle; preserved with benzoic acid at room temp. for several days
8. Nasal Solutions
-administered in drops/sprays; ex.:
a. Ephedrine- decongestant
b. Lypressin- diabetes insipidus
c. Oxytocin- milk letdown
d. Bricanyl (Terbutaline)
e. Ventolin (Salbutamol)

9. Otic/ Aural Solutions

-main solvents: water or glycerin (highly viscous so drug remain in ear)
-must have surfactants to remove cerumen; ex.:
a. Benzocaine Otic Solution
b. Neomycin+Polymyxin B Sulfate+Hydrocortisone Otic Solution
10. Irrigation Solutions
11. Sweet & Viscid Preparations
1.) Syrups
-concentrated or nearly saturated solutions of sugar

-viscosity enhancers: glycerin, sorbitol

>> Types of Sugars:
1. Simple Syrup/ Syrup NF: 85%w/v or 65%w/w sucrose
(<mentioned conc. will require preservative); spGr
of 1.313
2. Flavored Syrup: with juice or flavorant
3. Medicated Syrup: with AI
>> Method of Preparation:
1. Solution with heat: usual method; rapid process
2. Agitate without heat: when theres volatile substance
3. Reconstitution: adding medicating liquid to syrup
4. Percolation: an aqueous solution or water pass slowly
(1mL/min) through bed of crystalline sucrose; rapid
lead to bubbles & oxidation

flow
2.) Honeys

-thick; instead of syrup, honey is used as base; ex.:

a. Squill Oxymel: by maceration; squill+water+acetic
acid+honey

3.) Mucilages
-thick, viscid, adhesive, ex.:
a. Acacia Mucilage: contain benzoic acid
b. Tragacanth Mucilage: contain alcohol+ chloroform water
>> Method of Preparation:
1. Disperse gum in water
2. Extract mucilage from vegetable substance with water
4.) Jellies
-class of gels with high portion of liquid (usually water) in its matrix

B. NON-AQUEOUS SOLUTIONS
1. Alcoholic & Hydroalcoholic Solutions
1.) Elixir
- hydroalcoholic; clear, flavored, sweetened; for oral use
>>Types of elixirs:
1. Low alcoholic Elixir: 8-10% alcohol
2. Elixirs with 10-12% alcohol: self-preserving
3. High alcoholic elixirs: 75-78% alcohol
4. Iso-alcoholic elixir: mixture of high & low; vehicle for drugs
requiring solvents of different alcoholic
concentrations
2.) Spirits/ Essences
-alcoholic/ hydroalcoholic with volatile substance
>>Method of preparation:

1. Simple Solution: most common; ex.: Aromatic Ammonia Spirit

2. Solution with Maceration: Peppermint Spirit
3. Solution by Chemical Reaction: Ethyl Nitrite Spirit
4. Distillation: Brandy (vinivitus/ripe grapes) & Whisky (malt)
2. Oleaginous Solutions
1.) Oleovitamins
-fish liver oil diluted with edible vegetable oil, or, vitamin concentrates
(usually A & D) in fish liver oil
2.) Liniments/ Embrocations
-various substances in oil, alcoholic solution of soaps, or emulsion
-may contain antimicrobial preservatives
>>Types of liniment:
1. Oily: for massage
2. Alcoholic: rubefacient, counterirritant, mildly astringent,
penetrating
3.) Toothache Drops
-temporary relief; saturate small cotton, apply to cavity; composed by:
a. Anesthetics: Eugenol (clove oil), Benzocaine
b. Other ingredients: Camphor, Creosote, Menthol, Alcohol
3. Ethereal Solutions
1.) Pyroxilin/Soluble Gun Cotton/Collodion Cotton/Nitrocellulose
-from reaction of HNO3 + H2SO4 on cotton; chiefly composed of
cellulose tetranitrate
2.) Collodions
-pyroxylin in alcohol+ether (1:3) mixture; medicinal agent; ex.:
a. Flexible Collodion: with 2% Camphor (waterproof) & 3%
Oil (flexible)

Castor

b. Salicylic Acid Collodion: 10% salicylic acid solution in flexible

collodion; keratolytic
II. EMULSION
>METHODS OF PREPARATION:
1. Dry-Gum/ Continental/ 4:2:1
-4:2:1 O:W:G; order of mixing is (O+G) + W
2. Wet-Gum/ English
-same as dry-gum but different order: (W+G) + O slowly in portions
3. Bottle/ Forbes Bottle
-for extemporaneous preparation of emulsion from volatile or oleaginous
substance of low viscosity
- 3:2:1 or 2:2:1 O:W:Emulsifier
4. Nascent/ In-situ Soap
-aqueous solution of alkali + oil; emulsifying agent is the salt of free fatty acid

>REASONS FOR EMULSION:

>2 PHASES:

Appearance
Prolong Action
Solubility/ Absorption
Stability
Taste

1. Internal/ Dispersed/ Discontinuous

2. External/ Dispersion/ Continuous
>TYPES:
1. O/W
2. W/O
3. Multiple (OWO or WOW)
4. Micro-emulsion -most stable; single phase

>TESTS APPLIED:
1. Dilution
2. Dye Solubility
3. Electric Conductivity
4. Fluorescence
>EMULSIFYING AGENTS:
-maintain integrity; prevent coalescence; forms film at interface to lower tension
a. Base on function
1. True/ Primary: can stabilize themselves
2. Stabilizers/ Auxillary: needs primary agent
b. Base on source
1. Natural: acacia, tragacanth, gelatin, agar, pectin
2. Synthetic:
a. Anionic: sulfuric acid esters (Na lauryl sulfate)
b. Cationic: quaternary ammonium compounds (Benzalkonium Cl)
c. Non-ionic:
1. Spans (sorbitan esters) for w/o
2. Tweens (polysorbates) for o/w
III. SUSPENSIONS
>REASONS FOR SUSPENSIONS:

For solutes insoluble & unstable in solution form

Mask Taste

>PROBLEMS IN FORMULATION:
1. Caking: cement-like; small particles fill inter-particle spaces
2. Inaccurate dose: remedied by using measuring cup
>TYPES:
1. Gels
-semisolid; either small inorganic or large organic molecules interpenetrated
by a liquid; ex.:
a. Aluminum Hydroxide Gel: antacid
b. Betamethasone Gel: anti-inflammation
c. Tretinoin Gel: keratolytic
2. Lotions
-suspension or dispersion; external use
>>Methods of preparation:

ZnO +

1. Trituration: porcelain mortar for efflorescent & deliquescent; glass

for substances that stain, ex. Calamine Lotion:
ferric oxide (aesthetic use)

2. Chemical Reaction: ex. White Lotion: ZnO + sulfurated potash

3. Magma/ Milk
-suspension of insoluble, inorganic; suspended particles are larger than in gel
>>Methods of preparation:
1. Hydration: ex. Milk of Magnesia- laxative & antacid
2. Chemical Reaction: ex. MgSO4 + NaOH Mg(OH)2
4. Mixtures
-oral liquids with AI; dissolved, suspended, or dispersed, ex.:
a. Kaopectate: antidiarrheal (kaolin+ pectin)
b. Bordeaux Mixture: algaecide in pools (CuSO4+CaO)
>SUSPENDING AGENTS:
1. Hydrophilic Colloids: Tracaganth
2. Clays: Bentonite, Veegum
3. Agar & Pectin

IV. EXTRACTIVES
>METHODS OF EXTRACTION:
1. Maceration
-in stoppered container; 3 days in warm place; frequent agitation
2. Digestion
-maceration but with gentle heat
3. Infusion
-maceration in hot or cold H2O
4. Percolation
-evenly & uniformly damp; 15 mins then transferred to percolator and
packed; add solvent to saturate drug; macerate for 1 day or as
specified
5. Decoction
-boiling in water for 15 mins; for water-soluble & heat-stable
>TYPES:
1. Tinctures
-alcoholic/ hydroalcoholic; from vegetable or chemical
-potent (10g/100ml or 10%w/v)
>>Methods for Tincture:
1. Process P/ Percolation: Belladona Tincture
2. Process M/ Maceration: Sweet Orange Peel Tincture
3. Simple Solution: Iodine Tincture (2% I in 50% alcohol)
2. Fluidextracts
-vegetable drug + alcohol as solvent and/or preservative
-1g/1mL or 100%
>> Methods for Fluidextract:
1. Process A/ Percolation
2. Process E: alternative of A; drug column used is length>diameter

3. Process D: menstruum is boiling H2O: Cascara Sagrada Fluid Extract

(cathartic)
3. Extracts
-vegetable or animal; obtained by:
1. Removal of AI with suitable menstruum
2. Evaporation of all (or nearly all) the solvent
3. Adjustment of residual mass to prescribed standard
>> 3 Forms of Extracts:
a. Semiliquid: syrupy
b. Solid/ Pillular: plastic mass; for making ointments & suppositories
c. Powdered: dry powder; for making tablets & capsules

SEMISOLID DF
I. OINTMENTS
-applied on skin or mucous membranes
>METHODS OF PREPARATION:
1. Incorporation: mix until uniform
2. Fusion: melted together, cooled with constant stirring until congealed
>BASES:
1. Oleaginous/ Hydrocarbon
-emollient, occlusive, ex.:
a. Petrolatum, USP (Yellow Petrolatum/Petroleum Jelly): Vaseline
b. White Petrolatum (White Petroleum Jelly): White Vaseline
c. Yellow Ointment (Simple Ointment)
d. White Ointment
2. Absorption
-emollient, less occlusive than oleaginous base; not easily removed
-permit incorporation of aqueous solutions to form W/O emulsion, ex:
a. Hydrophilic Petrolatum: permits small amount
b. Lanolin: permits additional amount
3. Water-Removable
-O/W emulsion resembling creams; can absorb serous discharge; washable
-may be diluted with aqueous solutions or water, ex:
a. Hydrophilic Ointment
4. Water-Soluble
- no oleaginous component; greaseless; completely washable
-soften greatly with water; large amount of aqueous solutions not permitted
-for incorporation of solid substances, ex:
a. PEG Ointment
<600 MW:
600-1000 MW:
>1,000 MW:
II. CREAMS

clear liquid
semisolids
wax-like, white

-AI dissolved or dispersed in O/W or W/O emulsion or in another type of water-washable

base, ex:
a. Vanishing Cream (O/W)
b. Cold Cream (W/O)
III. PASTES
-applied on skin except hairy parts; contain greater amount of solid material (25%) than
ointment; stiffer; remains in place
-absorb serous discharge; ex.:
a. ZnO Paste/ Lassars Plain Zn Paste: (25% ZnO + 25% Starch) + White Petrolatum

IV. PLASTERS
-solid or semisolid adhesive mass on back of Paper/ Plastic/ Fabric/ Moleskin
-applied to prolong contact at site; ex.:
a. Salicylic Acid Plaster: 10-40% salicylic acid
V. GLYCEROGELATINS
- plastic mass; contains:
1. 40% glycerin
2. 35% water
3. 15% gelatin
4. 10% medicinal substance
- applied on skin with fine brush, ex.:
a. Zinc Gelatin/ Zinc Gelatin Boot: for varicose ulcers
SPECIAL DF
I. RADIOPHARMACEUTICALS
-Curie (Ci): fundamental unit; 3.7 x 1010 nuclear transformation/sec or disintegrations/sec
(DPS)
-Becquerel (Bq): international unit; 1 DPS
*1 milli Ci (mCi)= 37 MegaBq (MBq)
II. AEROSOLS
-dispersion of liquid/solid materials in gaseous medium
-depends on power of liquefied/compressed gas to dispense as mist, foam, or semisolid
>Metered Dose Inhalers (MDI)
-administration of fine solid or liquid mist via respiratory system or nasal passages
-used when drug is potent; particles are <10m (3-6 m: max therapeutic response)
>ADVANTAGES:

Allow dose titration

Alternate route
Ideal for PRN
No 1st-Pass
Rapid onset

>BASIC PARTS OF AEROSOL:

1. Propellant- force to expel; acts as solvent & diluent
a. Compressed Gases: CO2, NO(NITROUS), N
b. Liquefied Gases: saturated HC (n-butane, propane), CFCs, HCFs (preffered
than CFCs), dimethyl ether
2. Container
a. Tin-plated Steel: most used metal container; light & cheap
b. Aluminum: preffered for MDI; strong, less reactive vs. other metals

c. Glass: uncoated or plastic coated; limited to low pressure & propellant

percentage; high aesthetic value, minimal incompatibilities
3. Valve- most basic part; spray or foam; where content is emitted; regulates flow
4. Actuator- allows product to be dispensed in rapid, convenient, desired form
5. Dip tube- conveys liquid from bottom to top (valve); prevent escape of propellant
>TYPES:
1. Solution- in pure propellant & solvents
2. Dispersion/ Suspension/ Powder- like solution, but AI is suspended/dispersed; fpr
difficult to dissolve compound, ex: antibiotics & steroids
3. Emulsion-as stable foam, quick-breaking foam, or spray; O/W or W/O
4. Semisolid- depends on Nitrogen to push contents